光交联聚酯微针作为药物持续释放系统用于增生性疤痕治疗。

IF 6.5 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Drug Delivery Pub Date : 2024-12-01 Epub Date: 2024-02-29 DOI:10.1080/10717544.2024.2305818
Anna Szabó, Ignace De Decker, Sam Semey, Karel E Y Claes, Phillip Blondeel, Stan Monstrey, Jo Van Dorpe, Sandra Van Vlierberghe
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引用次数: 0

摘要

烧伤会导致严重的炎症反应,通常会形成增生性瘢痕(HTS)。建议采用皮质类固醇注射等局部药物疗法来治疗 HTS,但这些疗法具有创伤性、依赖操作者、极其痛苦,而且不能延长药物释放时间。基于聚合物的微针(MN)阵列可作为标准疗法的可行替代方案,同时还能直接、无痛地在皮肤上给药,并可定制药物释放曲线。在本研究中,我们合成了可光交联、丙烯酸酯末端包覆的聚氨酯基聚(ε-己内酯)(AUP-PCL),用于制造微针。对开发的聚合物进行了物理化学表征(1H-NMR、溶胀评估、凝胶分数),证实 PCL-二醇的丙烯酸化成功。随后,制备了 AUP-PCL 和市售 PCL 微针阵列,以对构建物进行比较评估。氢化可的松被选为模型药物。为了提高微针的药物释放效率,使用了非离子表面活性剂 Brij®35。通过差示扫描量热法评估了 MNs 的热性能。对阵列进行的压缩测试证实,在施加 7 N 的负荷时,MNs 保持完好无损,这与 MNs 的标准真皮插入力相关。对阵列的药物释放情况进行了评估,结果表明所开发的 PCL 阵列可提供长达两天的高效药物释放,而 AUP-PCL 阵列可提供长达三周的药物释放。最后,将 MN 阵列插入皮肤样本,然后进行组织学分析,结果表明 AUP-PCL MN 在皮肤表皮层形成金字塔形穿孔的效果优于 PCL 阵列。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Photo-crosslinkable polyester microneedles as sustained drug release systems toward hypertrophic scar treatment.

Burn injuries can result in a significant inflammatory response, often leading to hypertrophic scarring (HTS). Local drug therapies e.g. corticoid injections are advised to treat HTS, although they are invasive, operator-dependent, extremely painful and do not permit extended drug release. Polymer-based microneedle (MN) arrays can offer a viable alternative to standard care, while allowing for direct, painless dermal drug delivery with tailorable drug release profile. In the current study, we synthesized photo-crosslinkable, acrylate-endcapped urethane-based poly(ε-caprolactone) (AUP-PCL) toward the fabrication of MNs. Physico-chemical characterization (1H-NMR, evaluation of swelling, gel fraction) of the developed polymer was performed and confirmed successful acrylation of PCL-diol. Subsequently, AUP-PCL, and commercially available PCL-based microneedle arrays were fabricated for comparative evaluation of the constructs. Hydrocortisone was chosen as model drug. To enhance the drug release efficiency of the MNs, Brij®35, a nonionic surfactant was exploited. The thermal properties of the MNs were evaluated via differential scanning calorimetry. Compression testing of the arrays confirmed that the MNs stay intact upon applying a load of 7 N, which correlates to the standard dermal insertion force of MNs. The drug release profile of the arrays was evaluated, suggesting that the developed PCL arrays can offer efficient drug delivery for up to two days, while the AUP-PCL arrays can provide a release up to three weeks. Finally, the insertion of MN arrays into skin samples was performed, followed by histological analysis demonstrating the AUP-PCL MNs outperforming the PCL arrays upon providing pyramidical-shaped perforations through the epidermal layer of the skin.

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来源期刊
Drug Delivery
Drug Delivery 医学-药学
CiteScore
11.80
自引率
5.00%
发文量
250
审稿时长
3.3 months
期刊介绍: Drug Delivery is an open access journal serving the academic and industrial communities with peer reviewed coverage of basic research, development, and application principles of drug delivery and targeting at molecular, cellular, and higher levels. Topics covered include all delivery systems including oral, pulmonary, nasal, parenteral and transdermal, and modes of entry such as controlled release systems; microcapsules, liposomes, vesicles, and macromolecular conjugates; antibody targeting; protein/peptide delivery; DNA, oligonucleotide and siRNA delivery. Papers on drug dosage forms and their optimization will not be considered unless they directly relate to the original drug delivery issues. Published articles present original research and critical reviews.
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